I-Vildagliptin: i-analogues nentengo, imiyalo yokusebenzisa noGalvus noMetformin

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Abantu abahlushwa isifo sohlobo lwe-2 mellitus abakwazi ukuhlala begcina amazinga kashukela ezingeni elijwayelekile ngenxa yomsebenzi owodwa womzimba nokudla okukhethekile okufaka ngaphandle carbohydrate namafutha kalula.

Lokhu kwenzeka kaningi ngenqubo ende yesifo, ngoba minyaka yonke amandla okusebenza kwamanyikwe awohloka. Ngemuva kwalokho amaphilisi we-Galvus asiza, anciphisa futhi abambezele ushukela ngaphakathi kwamanani ajwayelekile.

Abaningi besifo sikashukela banesifiso sokuthi umuthi ophethe i-vildagliptin usebenza kangakanani. Ngakho-ke, le ndatshana izembula indlela yokusebenza kwento nalokho okusebenziseka kukho, ukuze wonke umuntu azenzele ngokwakhe usizo lomuthi we-hypoglycemic.

Isenzo se-Pharmacological

IVildagliptin (Uhlobo lwesiLatini - i-Vildagliptinum) kungokwesigaba sezinto ezikhuthaza izichibi zeLangerhans emanyikweni futhi zivimbele umsebenzi we-dipeptidyl peptidase-4. Umphumela wale enzyme ubhubhisa uhlobo lwe-1 glucagon-peptide (GLP-1) ne-glucose-insulinotropic polypeptide (HIP).

Njengomphumela, isenzo se-dipeptidyl peptidase-4 sicindezelwa yinto, futhi ukukhiqizwa kwe-GLP-1 ne-HIP kuyathuthukiswa. Lapho ukuqina kwegazi labo kukhuphuka, i-vildagliptin ithuthukisa ukuzwela kwamangqamuzana e-beta kushukela, okwandisa ukukhiqizwa kwe-insulin. Izinga lokukhuphuka kokusebenza kwamaseli we-beta lincike ngqo kuzinga lomonakalo wabo. Ngakho-ke, kubantu abanamanani ajwayelekile kashukela lapho besebenzisa izidakamizwa eziqukethe i-vildagliptin, lokho akukuthinti ukukhiqizwa kwama-hormone anciphisa ushukela futhi, ne-glucose.

Ngaphezu kwalokho, lapho umuthi unyusa okuqukethwe kwe-GLP-1, ngasikhathi sinye, ukuzwela kweglucose kuyanda kumaseli we-alpha. Inqubo enjalo ifaka ukwanda emithethweni elawulwa yiglucose yokukhiqizwa kwamangqamuzana ama-alpha alpha, abizwa ngokuthi yi-glucagon. Ukwehlisa okuqukethwe kwayo okunyukayo ngesikhathi sokusetshenziswa kwezitsha kusiza ukuqeda ukungatheleleki kweseli kwi-insulin ye-hormone.

Lapho isilinganiso se-insulin ne-glucagon sikhuphuka, okunqunywa inani elikhulayo le-HIP ne-GLP-1, esimweni se-hyperglycemic, ushukela esibindini uqala ukukhiqizwa ngezinga elincane, kokubili ngesikhathi sokudla kokudla nangemva kwalo, okubangela ukwehla kokuqukethwe kwe-glucose ku-plasma yegazi yesifo sikashukela.

Kumele kuqashelwe ukuthi, usebenzisa iVildagliptin, inani lamalipids liyancipha ngemuva kokudla. Ukwanda kokuqukethwe kwe-GLP-1 kwesinye isikhathi kubangela ukwehla kokukhishwa kwesisu, yize umphumela onjalo ungatholakalanga ngesikhathi sokufakwa.

Ucwaningo lwakamuva oluhilela cishe iziguli ezingama-6,000 emasontweni angama-52 luveze ukuthi ukusetshenziswa kwe-vildagliptin kunganciphisa amazinga kashukela esiswini esingenalutho kanye ne-glycated hemoglobin (HbA1c) lapho kusetshenziswa umuthi:

  • njengesisekelo sokwelashwa ngezidakamizwa;
  • ngokuhlanganiswa ne-metformin;
  • kuhlangene ne-sulfonylureas;
  • ngokuhlanganiswa ne-thiazolidinedione;

Izinga le-glucose lehla ngokusetshenziswa okuhlanganisiwe kwe-vildagliptin nge-insulin.

Imiyalo yokusebenzisa amaphilisi

Emakethe yemithi, ungathola izidakamizwa ezimbili eziqukethe i-vildagliptin.

Umehluko usezigabeni ezisebenzayo: okokuqala, yi-vildagliptin kuphela, kuthi kwesesibili - vildagliptin, metformin.

Umenzi wemithi enjalo yinkampani yaseSwitzerland iNovartis.

Umuthi uyatholakala ngalezi zinhlobo ezilandelayo zomthamo:

  1. I-Vildagliptin ngaphandle kwezingxenye ezengeziwe (ezibhebheni izingcezu ezingama-28 kwiphakheji yama-50 mg);
  2. I-Vildagliptin ihlanganiswe neMetformin (amaphilisi angama-30 kwiphakheji engu-50/500, 50/850, 50/1000 mg).

Okokuqala, isiguli esinesifo sikashukela esingaxhomekeki ku-insulin kufanele sibonane nodokotela owelashayo ozobhala umuthi ngaphandle kokuhluleka. Ngaphandle kwalo, awunakuthola ikhambi. Ngemuva kwalokho isiguli kufanele sifunde ngokucophelela okufakwayo futhi, uma unemibuzo, buza udokotela wabo. Imiyalo yokusebenzisa umuthi iqukethe uhlu lwemithamo enconyiwe engashintshwa udokotela.

I-Vildagliptin 50 mg, njengethuluzi eliyinhloko, noma lihlanganiswe ne-thiazolidinedione, iMetformin noma i-insulin therapy, lithathwa kumthamo wansuku zonke we-50 noma 100 mg. Isifo sikashukela, okulesi sifo sithuthuka ngesimo esibi ngokwelashwa kwe-insulin, thatha u-100 mg ngosuku.

Inhlanganisela ephindwe kabili yezidakamizwa (i-vildagliptin ne-sulfonylurea derivatives) iphakamisa umthamo wansuku zonke we-50 mg ekuseni.

Inhlanganisela ephindwe kathathu yezidakamizwa, i.e. Vildagliptin, Metformin kanye nokuphuma kwe-sulfonylurea, kusikisela umthamo wansuku zonke we-100 mg.

Umthamo wansuku zonke we-50 mg usetshenziswa ngasese ekuseni, kanye ne-100 mg ngemithamo emibili ekuseni nakusihlwa. Ukulungiswa komthamo kubantu abanenkinga yokulimazeka okulinganiselwe noma okunempilo (ikakhulukazi, ngokuntuleka okungapheli) kungadingeka.

Umuthi ugcinwa endaweni engatholakali yezingane ezincane, ngamazinga okushisa angadluli ku-30C. Isikhathi sokugcina yiminyaka emi-3, lapho isikhathi esikhonjisiwe siphela, umuthi awukwazi ukusetshenziswa.

Contraindication kanye nomonakalo ongaba khona

IVildagliptin ayinakho ukuphikisana okuningi. Zihambisana nokungabekezelelani kwesiguli kokuthile okusebenzayo nakwezinye izakhi, kanye nokungabekezeleli kofuzo ku-galactose, ukuntuleka kwe-lactase kanye ne-glucose-galactose malabsorption.

Kufanele kukhunjulwe ukuthi ngenxa yokuntuleka kocwaningo, ukuphepha ukusebenzisa lo muthi ezinganeni nasebusheni (abangaphansi kweminyaka engu-18) akufundiswanga ngokuphelele.

Ayikho imininingwane yocwaningo ngokusetshenziswa kwe-vildagliptin ngesikhathi sokukhulelwa nokuncelisa, ngakho-ke ukusetshenziswa komuthi ngalesi sikhathi kwenqatshelwe.

Kuya ngokuthi i-Vildagliptin isetshenziswa njenge-monotherapy noma ngezinye izindlela, imiphumela emibi ehlukahlukene ingahle ibe khona:

  • i-monotherapy (Vildagliptin) - isimo se-hypoglycemia, ikhanda kanye nesiyezi, ukuqunjelwa, i-edema yangaphandle;
  • I-Vildagliptin, iMetformin - isimo se-hypoglycemia, ukuthuthumela, isiyezi kanye nekhanda;
  • I-Vildagliptin, i-sulfonylurea derivatives - isimo se-hypoglycemia, ukwethuka, isiyezi kanye nobuhlungu bekhanda, i-asthenia (ukuphazamiseka kwengqondo);
  • I-Vildagliptin, okususelwa ku-thiazolidinedione - isimo se-hypoglycemia, ukukhuphuka okuncane kwesisindo, i-edema yangaphakathi;
  • I-Vildagliptin, i-insulin (inhlanganisela noma ngaphandle kwe-metformin) - isimo se-hypoglycemia, ikhanda, i-gastroesophageal Reflux (ukuphonsa okuqukethwe esiswini emgodini), ukubanda, isicanucanu, ukwakheka ngokweqile kwegesi.

Ngesikhathi sokuhlola okwenziwe ngemuva kokumaketha, abanesifo sikashukela abaningi abathatha i-Vildagliptin baphawula ukusabela okunjalo okunjenge-hepatitis, urticaria, ukukhipha isikhumba, ukwakheka kwamabhlaza nokukhula kwesikhumba.

Noma kunjalo, yize lesi sidakamizwa sinohlu olubonakalayo lwemiphumela emibi, amathuba okuba khona kwawo mancane. Ezimweni eziningi, kungukungaphenduki okwesikhashana futhi ngisho nokubonakaliswa kwabo, ukuqedwa kokwelashwa akudingekile.

I-overdose nezincomo zokusetshenziswa

Ngokuvamile, i-Vildagliptin ibekezelelwa kahle yiziguli kumthamo wansuku zonke we-200 mg, kodwa akusekho okunye. Uma usebenzisa umthamo omkhulu kunalokho okudingekayo, kukhona okungenzeka okukhulu kwezimpawu zokweqisa komuthi.

Kumele kuqashelwe ukuthi lapho uyeka ukuthatha umuthi, zonke izimpawu zihamba.

Izimpawu zokweqisa ngokweqile zincike ngqo kusilinganiso sazo, isibonelo:

  1. Lapho kusetshenziswa ama-400 mg, ubuhlungu bemisipha, ukuvuvukala, ukudunwa kanye nokukhubazeka kwezinto ((amaphaphu kanye namafushane), ukukhuphuka kwesikhashana kokuqukethwe kwe-lipase. Futhi, izinga lokushisa lingakhuphuka kanye noshukela.
  2. Lapho usebenzisa ama-600 mg, ukuvela kwezandla nezinyawo kuyavela, kanye nokuqina kwawo nokuxhuga, ukwanda kokuqukethwe kwe-ALT, CPK, myoglobin, kanye ne-C-reactive protein.

Ekuqaleni kokwelashwa, udinga ukwenza izifundo zamakhemikhali we-biochemical wesibindi. Uma imiphumela ikhombisa ukwanda komsebenzi we-transaminase, ukuhlaziya kufanele kuphindwe futhi futhi kugijime njalo kuze kube yilapho izinkomba zizinza. Uma imiphumela yokuhlolwa ikhombisa umsebenzi we-ALT noma we-AST, ophindwe izikhathi ezi-3 kune-VGN, umuthi uzokhanselwa.

Uma isiguli sephula isibindi (ngokwesibonelo, i-jaundice), ukusetshenziswa kwalesi sidakamizwa kuyeka ngokushesha. Ngenkathi isibindi singafani, ukwelashwa akuvunyelwe.

Lapho ukwelashwa kwe-insulin kudingeka, i-vildagliptin isetshenziswa kuphela nge-hormone. Futhi, ukusetshenziswa kwayo akunconywa kakhulu ekwelapheni izinhlobo zokuncika ezingena-insulin sikashukela (uhlobo 1) noma ukuphazamiseka kwe-carbohydrate metabolism - diabetes ketoacidosis.

Amandla we-vildagliptin ukuthonya ukunaka ukunakwa awaqondakali ngokuphelele. Kodwa-ke, uma kwenzeka isiyezi, iziguli ezishayela izimoto noma zenza omunye umsebenzi ngezindlela kudingeka ziwushiye lowo msebenzi oyingozi isikhathi sokwelashwa.

Izindleko, ukubuyekezwa kanye nama-analogues

Njengoba i-Vildagliptin yezidakamizwa ingenisiwe (umakhi waseSwitzerland), ngakho-ke intengo yayo ngeke ibe ngaphansi kakhulu. Noma kunjalo, noma yisiphi isiguli esinomholo ophakathi singawukhokhela umuthi. Ithuluzi lingathengwa ekhemisi noma liyalwe online.

Izindleko zomuthi (izibhebhe ezingama-28 zamathebulethi angama-50 mg) ziyahlukahluka kusuka ku-750 kuya kuma-880 ama-ruble aseRussia.

Ngokuqondene nemibono yodokotela neziguli maqondana nokusetshenziswa komuthi, ukubukeza kulungile kakhulu.

Iziguli ezinesifo sikashukela i-mellitus zohlobo lwesibili ezithathe amaphilisi ziveza izinzuzo ezilandelayo zomuthi:

  • ukwehla okusheshayo koshukela nokulugcina luphakathi kwemikhawulo ejwayelekile;
  • ukusetshenziswa kalula kwefomu lomthamo;
  • ukubonakaliswa okungatholakali kakhulu kokusabela okungalungile kwesidakamizwa.

Ngokusekelwe kulokhu, umuthi ungabhekwa njengomuthi osebenzayo we-hypoglycemic ekulweni nesifo sikashukela sohlobo 2. Kepha kwesinye isikhathi maqondana ne-contraindication noma ukulimala okungenzeka, kufanele wenqabe ukusebenzisa umuthi. Ezimweni ezinjalo, uchwepheshe owelapha unikeza ama-analogues - ama-ejenti anomphumela ofanayo wokwelapha njengoVildagliptin. Lokhu kufaka phakathi:

  1. Onglisa. Into esebenzayo yi-saxagliptin. Izindleko ziyehluka ngomkhawulo wama-ruble ayi-1900.
  2. I-Trazenta. Isithako esisebenzayo yi-linagliptin. Intengo emaphakathi ama-ruble ayi-1750.
  3. UJanuvius. Into esebenzayo yi-sitagliptin. Izindleko ezijwayelekile ama-ruble ayi-1670.

Njengoba ukwazi ukubona, ama-analogue aqukethe izakhi ezahlukahlukene ekwakhekeni kwazo. Kulokhu, udokotela kufanele akhethe umuthi onjalo ukuze ungabangeli ukusabela okungesihle esigulini. Kumele kuqashelwe ukuthi ama-analogues akhethwe ngokuya ngesisekelo sentengo, nayo idlala indima ebalulekile.

Umuthi i-Galvus vildagliptin (isiLatini - i-Vildagliptinum), ungabhekwa njengesidakamizwa esisebenzayo se-hypoglycemic, esithathwa njengesisekelo futhi sihlanganiswa nezinye izidakamizwa. Isibonelo, inhlanganisela ye-vildagliptin, i-metformin ene-sulfonylurea derivatives. Ukusetshenziswa okuzimele kwesidakamizwa akuvunyelwe, kufanele ngaso sonke isikhathi unamathele ezincomweni zikadokotela. Uma kunjalo, uma umuthi ungeke uthathwe ngenxa yesizathu esithile, udokotela unquma i-analogues. Ividiyo ekulesi sihloko izoqhubeka nesihloko somuthi wesifo sikashukela.

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